Guest guest Posted November 22, 2003 Report Share Posted November 22, 2003 This taken from article under this post.... Naltrexone for cancer is used at 3 mg per day, once a day, at bedtime. Since the drug only comes in 50 mg pills, a compounding pharmacy has to grind the pill down and make low dose pills. Dr Bihari feels that these pills are more stable than liquid made from the 50 mg pill. There are a number of pharmacies around the country that make it available. Check with your local compounding pharmacy, or try Apothecure at 1-800-969-6601, or Pharmacy at 603-539-2020. (Dr. B now gives 4.5 for cancer) Contents: Overview Pharmacology Patient experience References Overview Naltrexone is a commercially avaliable prescription drug, approved by the FDA since the early 1980s, which is manufactured by DuPont and made available under the trade name of ReVia. It has been used for a number of years as an adjunct to the treatment of opioid addictions, and sometimes alcoholism as well. There has been off-label experimenation with this drug for other purposes, namely in the treatment of autism, obesity, and certain types of cancer. Naltrexone blocks opioid receptors on the surface of cells. As a result, opiates will not produce euphoria and their effect on pain may be less predictable. It is thought that when very small doses are used, naltrexone will increase natural endorphins in the body which play a role not only in mood regulation but also in the level of immune functioning. Two physicians have experimented with the use of naltrexone in cancer: Dr Bihari in NYC, and Dr Margaret Lewin, an oncologist at New York Hospital-Cornell Medical Center. Dr Bihari looked for an opiod antagonist when he realized this could boost the immune functioning of his AIDS patients. When he got good results with it, he then postulated that certain cancers that have plenty of opioid receptors in their cells, could also be influenced by this drug. He suggested it in 1993 to Dr Lewin who has tried it in a few patients with lymphoma. Early research showed that heroin inhibits the growth of certain tumors, and that a certain endorphin called metenkephalin prolongs the survival of mice with leukemia, melanoma, and other cancers. Further research found that opiate receptors play a key role in the action of these endorphins. Naltrexone was used in these studies. Other studies showed that high doses of naltrexone stimulated tumor growth, and very small doses prolong survival in mice with cancer, and protect those mice at risk of developing cancer. It was noted that opiate peptides play a key role in regulating the growth of certain cancers, and then hypothesized that small daily doses of naltrexone would enhance the protective effect of endorphins by increasing the number and density of opiate receptors on tumor cells. The effects of the endorphins are thought to work against the cancer cells indirectly by inhibiting their DNA synthesis and mitosis, and other subtle changes. There is a significant body of literature that suggested to Dr Bihari that endorphins are very involved in the regulation of immune function, and led to his initial experimentation with HIV positive patients. He and his colleagues found that low dose naltrexone increases beta-endorphins in healthy volunteers within 2 hours, with a greater rise some 12-16 hours later if the dose was given in the late evening. Their 12 week placebo controlled trial in AIDS patients showed decline in the levels of alpha interferon and better protection against opportunistic infections (no patients of 22 in the active arm developed infections, while 5 of the 16 placebo arm patients did). Another placebo controlled trial showed a significant increase in NK (natural killer) cells, as well as lymphomcytes and CD4s. Dr Bihari thinks that naltrexone may work in the following ways: by increasing the endorphin levels, by increasing opiate receptors in tumor cell membranes and thus making the cells more susceptible to endorphin effects, and by increasing the levels of NK cells and their activity. The cancers thought most responsive to low dose naltrexone originate in tissues with high densities of opioid receptors, particularly lymphomas (including Hodgkin's disease, NHL, CLL, and multiple myeloma) and cancer of the pancreas. Other cancers also quite high in these receptors are colorectal cancers, metastatic melanoma, neuroblastoma, glioma, cancer of the small intestine, prostate cancer, and some endocrine cancers. Dr Bihari began to use naltrexone in cancer in 1985 in a patient with NH lymphoma that recurred and the patient refused further chemo. Her large groin tumors regressed within 12 weeks and she died 4 years later of an unrelated cause while still in remission. Dr Bihari introduced Dr Lewin to naltrexone in 1993, and she has apparently been using it in her practice with some cancer patients who have exhausted mainstream treatments. An indetermined percentage ("sizable minority") of these patients have had success with it, and Dr Lewin has been reported to say she considers the results "suggestive." She has not used it with untreated patients. Naltrexone for cancer is used at 3 mg per day, once a day, at bedtime. Since the drug only comes in 50 mg pills, a compounding pharmacy has to grind the pill down and make low dose pills. Dr Bihari feels that these pills are more stable than liquid made from the 50 mg pill. There are a number of pharmacies around the country that make it available. Check with your local compounding pharmacy, or try Apothecure at 1-800-969-6601, or Pharmacy at 603-539-2020. Back to top Pharmacology Pharmaceutical information on naltrexone hydrochloride can be found in the Physicians' Desk Reference (also available in public libraries). It is classified as a pure opioid antagonist. It will block physical dependence on opiate drugs like heroin, morphine et al. It will cause withdrawal symptoms in people habituated to these substances. It is mostly eliminated by the kidneys. Some of it is recycled by the liver. It is rapidly absorbed after ingestion, mostly from the GI tract. Peak plasma levels occur about 1 hour after dosing, and the effect lasts 24-72 hours. While seemingly safe at low levels, it has been shown to be a hepatotoxin (liver poison) at dosages of about 300 mg per day in healthy volunteers. Its effects in pregnancy and lactation has not been studied. Studies in patients who have severely compromised liver and kidney function have not been conducted. Its safety in children has not been established. It is used at 5o mg per day for its approved use in opioid addiction. Side effects reported at these levels: GI upset in about 15 % of patients, Contraindicated in patients who are using opioid pain killers, patients with a history of sensitivity to naltrexone, patients with acute hepatitis or liver failure. It has the capacity to cause hepatocellular injury if given in excessive doses (about 5 times or less). It does not appear to be a hepatotoxin at 50 mg per day. If a patient must receive opioid analgesics while using naltrexone, the amount required may need to be adjusted upward, and careful monitoring is required. Patients are advised to look for signs of liver toxicity when using this product: white stools, dark urine, yellowing of eyes, or ongoing abdominal pain. Patients taking naltrexone may not benefit from opiate-containing medicines such as cough syrups, cold and antidiarrheal preparations, and opioid analgesics. In carcinogenesis studies on rodents, there was a small increase in mesotheliomas and vascular tumors. Other rare side effects include: tearfulness, dizziness, mild nausea, abdominal cramps, restlessness, body or muscle pains, and sinus problems. Volunteers who took 800 mg over a week showed no signs of overdose. Deaths in animals do not occur until the animal receives more than 1000 mg per kg of weight. When considering the information on the side effects and its use in cancer, please remember that in cancer, the dosage is only 3 mg per day; this is only 6% of the customary prescription dose. Back to top Patient experiences Several lymphoma patients on the nhl-other list have begun to experiment with this substance, but it is too early to report any results. Please write of your experiences with lymphoma or other cancers and they will be added to the record here. Back to top Quote Link to comment Share on other sites More sharing options...
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